| Assay ID | Title | Year | Journal | Article |
|---|
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1625315 | Toxicity in human H3255 cells expressing L858R EGFR mutant xenografted in mouse administered ip 3 times per week | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
| Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions. |
| AID1759978 | Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Ring-opening of five-membered heterocycles conjugated 4-isopropylresorcinol scaffold-based benzamides as HSP90 inhibitors suppressing tumor growth in vitro and in vivo. |
| AID629846 | Binding affinity to human Hsp90beta assessed as dissociation constant after overnight incubation by fluorescence polarization assay | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone. |
| AID1167273 | Hepatotoxicity in Kunming mouse assessed as serum alanine aminotransferase level at 10 mg/kg, iv (Rvb = 60.7 +/- 6.9U/L) | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors. |
| AID1885315 | Inhibition of KDM4C (unknown origin) measured by AlphaScreen assay | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Recent Advances with KDM4 Inhibitors and Potential Applications. |
| AID288532 | Selectivity for HSP90 in MCF7 cells over HSP90 in NDF cells | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
| Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity. |
| AID1167286 | Cytotoxicity against human SW480 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors. |
| AID1740797 | Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Synthesis, structure and anticancer activity of new geldanamycin amine analogs containing C(17)- or C(20)- flexible and rigid arms as well as closed or open ansa-bridges. |
| AID1167280 | Cytotoxicity against HUVEC cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors. |
| AID1760055 | Therapeutic index, ratio of IC50 for HUVEC cells to IC50 for human A549 cells | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Ring-opening of five-membered heterocycles conjugated 4-isopropylresorcinol scaffold-based benzamides as HSP90 inhibitors suppressing tumor growth in vitro and in vivo. |
| AID1187086 | Antitumor activity against human MDA-MB-231 cells xenografted in BALB/c mouse assessed as tumor volume at 10 mg/kg, iv dosed every 3 days for 15 days relative to untreated control | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors. |
| AID629770 | Antiproliferative activity against human HL60 | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone. |
| AID1752529 | Toxicity in BALB/c mouse xenografted with mouse 4T1 cells assessed as effect on kidney morphology at 15 mg/kg, ip administered every 2 days starting from day 7 post-inoculation and measured on day 24 by Hematoxyin-eosin staining based analysis | 2021 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 50 | Total synthesis and biological evaluation of 7-hydroxyneolamellarin A as hypoxia-inducible factor-1α inhibitor for cancer therapy. |
| AID1755714 | Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-((1-Phenyl-1H-1,2,3-triazol-4-yl)methyl)-2-azabicyclo[3.2.1]octan-3-one derivatives: Simplification and modification of aconitine scaffold for the discovery of novel anticancer agents. |
| AID1755719 | Cytotoxicity against human L02 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-((1-Phenyl-1H-1,2,3-triazol-4-yl)methyl)-2-azabicyclo[3.2.1]octan-3-one derivatives: Simplification and modification of aconitine scaffold for the discovery of novel anticancer agents. |
| AID311910 | Displacement of fluorescent labelled VER-00051001 from human Hsp90-beta by FP assay | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
| 4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer. |
| AID1192910 | Inhibition of FITC-GA binding to Hsp90alpha (unknown origin) ATPase site after 2 hrs by fluorescence polarization assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Discovery of novel oxazepine and diazepine carboxamides as two new classes of heat shock protein 90 inhibitors. |
| AID324511 | Increase in light chain 3-GFP+ autophagosome vesicle area per cell in human H4 cells at 4.3 uM after 24 hrs by high throughput fluorescence microscopy relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
| Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
| AID443341 | Growth inhibition of human WS1 cells after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID506960 | Inhibition of HSP90-mediated antiapoptotic activity in human H69AR cells assessed as increase in caspase-3 activity at 10 uM after 48 hrs by Western blot analysis | 2007 | Nature chemical biology, Aug, Volume: 3, Issue:8
| Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. |
| AID1578155 | Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression. |
| AID1187085 | Antitumor activity against human MDA-MB-231 cells xenografted in BALB/c mouse assessed as reduction in tumor weight at 10 mg/kg, iv dosed every 3 days for 15 days | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors. |
| AID1185004 | Induction of apoptosis in human MIAPaCa2 cells assessed as caspase 3/7 activation at 1000 nM after 24 hrs by luminometry | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
| Chemically accessible hsp90 inhibitor that does not induce a heat shock response. |
| AID506969 | Inhibition of HSP90-mediated antiapoptotic activity in human H69AR cells assessed as increase in caspase-7 activity at 10 uM after 48 hrs by Western blot analysis | 2007 | Nature chemical biology, Aug, Volume: 3, Issue:8
| Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. |
| AID1310941 | Effect on cell cycle distribution in human MDA-MB-468 cells assessed as accumulation at G2/M-phase at 2 uM measured after 48 hrs by propidium iodide staining-based flow cytometry | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Novel 1,6-naphthyridin-2(1H)-ones as potential anticancer agents targeting Hsp90. |
| AID732371 | Inhibition of Hsp90 in human MCF7 cells assessed as decrease in Cdk4 level at 0.1 uM after 24 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Synthesis and biological activities of a new class of heat shock protein 90 inhibitors, designed by energy-based pharmacophore virtual screening. |
| AID1334310 | Inhibition of FITC-labeled geldanamycin binding to human Hsp90alpha by fluorescence polarization assay | 2017 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
| Synthesis and in vitro antiproliferative activity of C5-benzyl substituted 2-amino-pyrrolo[2,3-d]pyrimidines as potent Hsp90 inhibitors. |
| AID1708940 | Cytotoxicity in human CNE-2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
| Discovering High Potent Hsp90 Inhibitors as Antinasopharyngeal Carcinoma Agents through Fragment Assembling Approach. |
| AID314500 | Inhibition of Hsp90 in human KPL4 cells assessed as depletion of ErbB2 level after 40 hrs | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
| Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity. |
| AID314505 | Growth inhibition of human A549 cells | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
| Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity. |
| AID429791 | Growth inhibition of human MDA-MB-468 cells assessed as ATP level after 4 days | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID394599 | Binding affinity to human recombinant Hsp90alpha N-terminal domain by isothermal titration calorimetry | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
| AID1740804 | Selectivity index, ratio of IC50 for cytotoxicity against human HDF cells to IC50 for cytotoxicity against human PC-3 cells | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Synthesis, structure and anticancer activity of new geldanamycin amine analogs containing C(17)- or C(20)- flexible and rigid arms as well as closed or open ansa-bridges. |
| AID1187078 | Hepatotoxicity in Kunming mouse assessed as serum ALT level at 10 mg/kg, iv (Rvb = 60.7 +/- 6.9 U/L) | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors. |
| AID1187079 | Displacement of GA-FITC from human recombinant HSP90alpha ATP-binding site by fluorescence polarization assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors. |
| AID1625193 | Binding affinity to recombinant human HSP90 alpha by Surface plasmon resonance analysis | 2019 | Journal of natural products, 03-22, Volume: 82, Issue:3
| Fusicoccane Diterpenes from Hypoestes forsskaolii as Heat Shock Protein 90 (Hsp90) Modulators. |
| AID1167292 | Antitumor activity against human MDA-MB-231 cells xenografted in athymic nude mouse assessed as tumor growth inhibition at 10 mg/kg, iv dosed every 3 day for 15 consecutive days | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors. |
| AID506961 | Inhibition of HSP90-mediated antiapoptotic activity in human SKI-AC3 cells assessed as increase in caspase-3 activity at 10 uM after 48 hrs by Western blot analysis | 2007 | Nature chemical biology, Aug, Volume: 3, Issue:8
| Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. |
| AID421316 | Inhibition of Hsp90 in human AU565 cells assessed as pERK degradation after 24 hrs by high content screening | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. |
| AID1755707 | Cytotoxicity against human GES1 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-((1-Phenyl-1H-1,2,3-triazol-4-yl)methyl)-2-azabicyclo[3.2.1]octan-3-one derivatives: Simplification and modification of aconitine scaffold for the discovery of novel anticancer agents. |
| AID1726502 | Binding affinity to recombinant His6-tagged HSP90 NM-domain (unknown origin) (1 to 554 residues) expressed in Escherichia coli BL21 (DE3) (DNAY) cells by 15N-1H TROSY-HSQC NMR spectroscopy | 2021 | RSC medicinal chemistry, Mar-01, Volume: 12, Issue:3
| Using NMR to identify binding regions for N and C-terminal Hsp90 inhibitors using Hsp90 domains. |
| AID1167274 | Inhibition of GA-FITC binding to human recombinant Hsp90alpha incubated for 5 hrs by fluorescence polarization assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors. |
| AID115731 | In vivo inhibition of p185 phosphotyrosine in nu/nu nude mice bearing Fisher rat embryo cells transfected with human erbB-2 | 1995 | Journal of medicinal chemistry, Sep-15, Volume: 38, Issue:19
| erbB-2 oncogene inhibition by geldanamycin derivatives: synthesis, mechanism of action, and structure-activity relationships. |
| AID1578157 | Inhibition of FITC-geldanamycin binding to recombinant human full-length C-terminal His-tagged HSP90alpha expressed in Escherichia coli after 3 hrs by fluorescence polarization assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression. |
| AID1184986 | Induction of heat shock response in human MIAPaCa2 cells assessed as HSP70 protein expression at IC50 level by western blotting method relative to untreated control | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
| Chemically accessible hsp90 inhibitor that does not induce a heat shock response. |
| AID745563 | Cytotoxicity against human SMMC7721 cells after 48 hrs by MTS assay | 2013 | Journal of natural products, May-24, Volume: 76, Issue:5
| Cytotoxic bisbenzylisoquinoline alkaloids from Stephania epigaea. |
| AID1755721 | Cytotoxicity against human HPDE6c7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-((1-Phenyl-1H-1,2,3-triazol-4-yl)methyl)-2-azabicyclo[3.2.1]octan-3-one derivatives: Simplification and modification of aconitine scaffold for the discovery of novel anticancer agents. |
| AID1334307 | Growth inhibition of human HCT116 cells at 10 uM after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
| Synthesis and in vitro antiproliferative activity of C5-benzyl substituted 2-amino-pyrrolo[2,3-d]pyrimidines as potent Hsp90 inhibitors. |
| AID1755706 | Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-((1-Phenyl-1H-1,2,3-triazol-4-yl)methyl)-2-azabicyclo[3.2.1]octan-3-one derivatives: Simplification and modification of aconitine scaffold for the discovery of novel anticancer agents. |
| AID1192912 | Permeability across apical to basolateral side in MDCK-MDR1 cells | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Discovery of novel oxazepine and diazepine carboxamides as two new classes of heat shock protein 90 inhibitors. |
| AID1184982 | Induction of heat shock response in human HCT116 cells assessed as HSP40 protein expression at IC50 level by western blotting method relative to untreated control | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
| Chemically accessible hsp90 inhibitor that does not induce a heat shock response. |
| AID421313 | Antiproliferative activity against human K562 cells after 72 to 144 hrs by cyquant DNA dye method | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. |
| AID421300 | Inhibition of Hsp90 in human AU565 cells assessed as Her2 degradation after 24 hrs by high content screening | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. |
| AID429693 | Hepatotoxicity in ICR-SCID mouse liver assessed as aspartate aminotransferase level at 75 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID429782 | Toxicity in ICR-SCID mouse heart assessed as creatine phospholipase level at 50 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID1740802 | Selectivity index, ratio of IC50 for cytotoxicity against human HDF cells to IC50 for cytotoxicity against human SK-BR-3 cells | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Synthesis, structure and anticancer activity of new geldanamycin amine analogs containing C(17)- or C(20)- flexible and rigid arms as well as closed or open ansa-bridges. |
| AID506963 | Inhibition of HSP90-mediated antiapoptotic activity in human H69AR cells assessed as induction of caspase-3 cleavage at 10 uM after 48 hrs by Western blot analysis | 2007 | Nature chemical biology, Aug, Volume: 3, Issue:8
| Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. |
| AID392954 | Binding affinity to human Histidine6-tagged Hsp90alpha N-terminal domain expressed in Escherichia coli BL21 DE3 by ITC | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
| 5-Aryl-4-(5-substituted-2,4-dihydroxyphenyl)-1,2,3-thiadiazoles as inhibitors of Hsp90 chaperone. |
| AID1740803 | Selectivity index, ratio of IC50 for cytotoxicity against human HDF cells to IC50 for cytotoxicity against human SK-OV-3 cells | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Synthesis, structure and anticancer activity of new geldanamycin amine analogs containing C(17)- or C(20)- flexible and rigid arms as well as closed or open ansa-bridges. |
| AID429696 | Hepatotoxicity in ICR-SCID mouse liver assessed as alkaline phosphatase level at 50 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID394593 | Cytotoxicity against human SKBR3 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
| AID506971 | Inhibition of HSP90-mediated antiapoptotic activity in human WBA cells assessed as increase in caspase-7 activity at 10 uM after 48 hrs by Western blot analysis | 2007 | Nature chemical biology, Aug, Volume: 3, Issue:8
| Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. |
| AID394601 | Cytotoxicity against human SKOV3 cells after 72 hrs | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
| AID421304 | Antiproliferative activity against human LNCAP cells after 72 to 144 hrs by cyquant DNA dye method | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. |
| AID1720458 | Inhibition of HSP90 ATPase activity (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 30, Issue:15
| Quinazoline Based HSP90 Inhibitors: Synthesis, Modeling Study and ADME Calculations Towards Breast Cancer Targeting. |
| AID394605 | Cytotoxicity against NQ01-deficient human NCI-H596 cells after 72 hrs | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
| AID114897 | In vivo inhibition of phospho-p185erbB-2 expression in human SK-BR-3 tumors at 200 mg/kg dose in mice | 1995 | Journal of medicinal chemistry, Sep-15, Volume: 38, Issue:19
| Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives. |
| AID443312 | Inhibition of IP6K2 protein binding to human HSP90 isolated from Hela cells | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID612786 | Inhibition of human Hsp90 interaction with Her2 protein using coomassie staining by Western blotting | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
| Synthesis and evaluation of biotinylated sansalvamide A analogs and their modulation of Hsp90. |
| AID716076 | Inhibition of HSP90alpha in human MCF7 cells assessed as degradation of Her-2 | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| EC144 is a potent inhibitor of the heat shock protein 90. |
| AID1074619 | Inhibition of HSP90 in human CL1-5 cells assessed as reduction of phosphorylated Akt after 16 hrs by Western blotting analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
| The antitumor agent PBT-1 directly targets HSP90 and hnRNP A2/B1 and inhibits lung adenocarcinoma growth and metastasis. |
| AID394596 | Antitumor activity against human COLO205 tumor bearing mouse assessed as reduction of tumor volume at 90 mg/kg, iv administered once daily for 5 days with 2 day interval for total 13 doses | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
| AID1334311 | Inhibition of FITC-labeled geldanamycin binding to human Hsp90alpha at 10 uM by fluorescence polarization assay | 2017 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
| Synthesis and in vitro antiproliferative activity of C5-benzyl substituted 2-amino-pyrrolo[2,3-d]pyrimidines as potent Hsp90 inhibitors. |
| AID395891 | Inhibition of Her2 in human SKBR3 cells | 2009 | Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
| Discovery and development of heat shock protein 90 inhibitors. |
| AID1310947 | Inhibition of HSP90 in human MDA-MB-468 cells assessed as induction of prosurvival heat shock response at 0.5 uM measured after 48 hrs by Western blot analysis | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Novel 1,6-naphthyridin-2(1H)-ones as potential anticancer agents targeting Hsp90. |
| AID465299 | AUC in liver of mouse bearing human A2780 cells at 80 mg/kg, ip administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID767752 | Displacement of 5-(3-(3-(6-amino-8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9H-purin-9-yl)propyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from dog Grp94 after 24 hrs by fluorescence polarization assay | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series. |
| AID114899 | In vivo inhibition of phospho-p185erbB-2 expression in human SK-BR-3 tumors at 400 mg/kg dose in mice | 1995 | Journal of medicinal chemistry, Sep-15, Volume: 38, Issue:19
| Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives. |
| AID314503 | Growth inhibition of human HCT116 cells | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
| Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity. |
| AID621857 | Binding affinity to biotinylated N-terminal human HSP90alpha using of streptavidin coated surface by SPR binding assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
| Lead generation of heat shock protein 90 inhibitors by a combination of fragment-based approach, virtual screening, and structure-based drug design. |
| AID465318 | Toxicity in human assessed as maximum tolerated dose administered on daily schedule administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID288546 | Antitumor activity in human N87 cells xenografted mouse assessed as tumor growth inhibition at 90 mg/kg, ip administered weekly 5-day-on and 2-day-off schedule for 5 weeks | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
| Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity. |
| AID443324 | Growth inhibition of human HCT116 cells after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID247226 | Inhibition of HCT116 human colon cancer cell proliferation | 2005 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 15, Issue:14
| The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors. |
| AID1755718 | Cytotoxicity against human IOSE80 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-((1-Phenyl-1H-1,2,3-triazol-4-yl)methyl)-2-azabicyclo[3.2.1]octan-3-one derivatives: Simplification and modification of aconitine scaffold for the discovery of novel anticancer agents. |
| AID1578153 | Antiproliferative activity against human A549 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression. |
| AID421315 | Inhibition of Hsp90 in human A375 cells assessed as pS6 degradation after 24 hrs by high content screening | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. |
| AID465291 | Binding affinity to HSP90 by fluorescence polarization assay | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID1184988 | Induction of heat shock response in human MIAPaCa2 cells assessed as HSP27 protein expression at IC50 level by western blotting method relative to untreated control | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
| Chemically accessible hsp90 inhibitor that does not induce a heat shock response. |
| AID1310957 | Antiproliferative activity against human MCF7 cells measured after 5 days by MTS assay | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Novel 1,6-naphthyridin-2(1H)-ones as potential anticancer agents targeting Hsp90. |
| AID201637 | In vitro inhibition of phospho-p185erbB-2 expression in human breast cancer cells(SK-BR-3 cells) at 100 mg/kg dose. | 1995 | Journal of medicinal chemistry, Sep-15, Volume: 38, Issue:19
| Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives. |
| AID1740800 | Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Synthesis, structure and anticancer activity of new geldanamycin amine analogs containing C(17)- or C(20)- flexible and rigid arms as well as closed or open ansa-bridges. |
| AID114895 | In vivo inhibition of phospho-p185erbB-2 expression in human SK-BR-3 tumors at 100 mg/kg dose in mice | 1995 | Journal of medicinal chemistry, Sep-15, Volume: 38, Issue:19
| Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives. |
| AID1755750 | Antitumour activity against human SW-620 cells xenografted in Balb/c mouse assessed as inhibition of tumour growth at 5 mg/kg, ip measured after 21 days | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-((1-Phenyl-1H-1,2,3-triazol-4-yl)methyl)-2-azabicyclo[3.2.1]octan-3-one derivatives: Simplification and modification of aconitine scaffold for the discovery of novel anticancer agents. |
| AID1452316 | Inhibition of FITC-GA binding to N-terminal domain of HSP90alpha (unknown origin) after 5 hrs by fluorescence polarization assay | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design and synthesis of neolamellarin a derivatives targeting heat shock protein 90. |
| AID767753 | Displacement of 5-(3-(3-(6-amino-8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9H-purin-9-yl)propyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from recombinant HSP90beta (unknown origin) after 24 hrs by fluorescence polarization assay | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series. |
| AID1740801 | Cytotoxicity against human HDF cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Synthesis, structure and anticancer activity of new geldanamycin amine analogs containing C(17)- or C(20)- flexible and rigid arms as well as closed or open ansa-bridges. |
| AID443319 | Growth inhibition of human PL45 cells at 62.5 nM after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID429794 | Growth inhibition of human MV4-11 cells assessed as ATP level after 4 days | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID1728770 | Anti-necroptotic activity in human HT-29 cells assessed as inhibition of TNFalpha/SM-164/Z-VAD-fmk (TSZ)-induced necroptosis by measuring increase in cell viability at 10 uM measured after 12 hrs by celltiter-glo luminescent cell viability assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors. |
| AID465316 | Clearance in human at 220 mg/m2 administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID620121 | Inhibition of Hsp90alpha in human MCF7 assessed as induction of proteasomal ER2alpha protein degradation at 1 uM after 24 hrs by Western blot analysis relative to control | 2011 | Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
| Lead identification of β-lactam and related imine inhibitors of the molecular chaperone heat shock protein 90. |
| AID155500 | Inhibition of Phoshoinositol 3 kinase from MCF-7 breast cancer cells | 2001 | Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
| LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family. |
| AID394598 | Binding affinity to human recombinant Hsp90alpha N-terminal domain by scintillation proximity assay | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
| AID288531 | Binding affinity to HSP90 in human NDF cell lysates assessed as inhibition of biotinylated-geldanamycin binding | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
| Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity. |
| AID465289 | Binding affinity to HSP90 under reducing conditions in presence of TECP | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID1663548 | Antiproliferative activity against human CNE2Z cells assessed as cell growth inhibition by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 30, Issue:15
| Enzymatic biosynthesis and biological evaluation of novel 17-AAG glucoside as potential anti-cancer agents. |
| AID266549 | Inhibition of human SKOV3 cell growth | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
| Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. |
| AID1759975 | Antiproliferative activity against human A549 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Ring-opening of five-membered heterocycles conjugated 4-isopropylresorcinol scaffold-based benzamides as HSP90 inhibitors suppressing tumor growth in vitro and in vivo. |
| AID465315 | AUC in human at 220 mg/m2 administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID429793 | Growth inhibition of human K562 cells assessed as ATP level after 4 days | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID1708939 | Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
| Discovering High Potent Hsp90 Inhibitors as Antinasopharyngeal Carcinoma Agents through Fragment Assembling Approach. |
| AID1760003 | Cytotoxicity against mouse 661W cells by MTT based vision related toxicity assay | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Ring-opening of five-membered heterocycles conjugated 4-isopropylresorcinol scaffold-based benzamides as HSP90 inhibitors suppressing tumor growth in vitro and in vivo. |
| AID257070 | Binding affinity to Hsp90 by fluorescent polarization assay | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
| Structure-based discovery of a new class of Hsp90 inhibitors. |
| AID716012 | Cytotoxicity against human NCI-H295 cells overexpressing PGP xenografted in athymic mouse assessed as inhibition of tumor growth at 60 mg/kg, iv qd for 5 days per week for 4 weeks | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| EC144 is a potent inhibitor of the heat shock protein 90. |
| AID716033 | Toxicity in po dosed mouse administered as a single dose | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17
| EC144 is a potent inhibitor of the heat shock protein 90. |
| AID465312 | Cmax in human at 220 mg/m2 administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID604445 | Cytotoxicity against human SKBR3 cells | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors. |
| AID1167284 | Cytotoxicity against human A431 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors. |
| AID1740799 | Antiproliferative activity against human U-87 MG cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Synthesis, structure and anticancer activity of new geldanamycin amine analogs containing C(17)- or C(20)- flexible and rigid arms as well as closed or open ansa-bridges. |
| AID429704 | Toxicity in ICR-SCID mouse kidney assessed as BUN level at 50 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID745565 | Cytotoxicity against human HL60 cells after 48 hrs by MTS assay | 2013 | Journal of natural products, May-24, Volume: 76, Issue:5
| Cytotoxic bisbenzylisoquinoline alkaloids from Stephania epigaea. |
| AID1318682 | Antiproliferative activity against human HeLa cells after 72 hrs by SRB assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design and synthesis of N-(5-chloro-2,4-dihydroxybenzoyl)-(R)-1,2,3,4-tetrahydroisoquinoline-3-carboxamides as novel Hsp90 inhibitors. |
| AID604502 | Inhibition of Hsp90alpha in human SKBR3 cells assessed as ErbB2 degradation by Western blot analysis | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors. |
| AID664001 | Cytotoxicity against human NCI-H460 cells after 72 hrs | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Isoxazolo(aza)naphthoquinones: a new class of cytotoxic Hsp90 inhibitors. |
| AID604444 | Inhibition of Hsp90alpha ATPase activity by malachite green ATP-ase assay | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors. |
| AID266550 | Degradation of Her2 in SKBR3 cells | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
| Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. |
| AID612789 | Inhibition of human Hsp90 interaction with IP6K2 protein using coomassie staining by Western blotting | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
| Synthesis and evaluation of biotinylated sansalvamide A analogs and their modulation of Hsp90. |
| AID1184985 | Induction of heat shock response in human MIAPaCa2 cells assessed as HSP90 protein expression at IC50 level by western blotting method relative to untreated control | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
| Chemically accessible hsp90 inhibitor that does not induce a heat shock response. |
| AID1187077 | Hepatotoxicity in Kunming mouse assessed as serum AST level at 10 mg/kg, iv (Rvb = 197.2 +/- 11.2 U/L) | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors. |
| AID1310935 | Antiproliferative activity against human MDA-MB-468 cells measured after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Novel 1,6-naphthyridin-2(1H)-ones as potential anticancer agents targeting Hsp90. |
| AID503304 | Antiproliferative activity against human PC3 cells at 5 uM after 120 hrs by MTT assay relative to DMSO | 2006 | Nature chemical biology, Jun, Volume: 2, Issue:6
| Identifying off-target effects and hidden phenotypes of drugs in human cells. |
| AID486953 | Inhibition of HSP90 | 2010 | European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
| 3D QSAR pharmacophore based virtual screening and molecular docking for identification of potential HSP90 inhibitors. |
| AID1752530 | Toxicity in BALB/c mouse xenografted with mouse 4T1 cells assessed as effect on heart morphology at 15 mg/kg, ip administered every 2 days starting from day 7 post-inoculation and measured on day 24 by Hematoxyin-eosin staining based analysis | 2021 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 50 | Total synthesis and biological evaluation of 7-hydroxyneolamellarin A as hypoxia-inducible factor-1α inhibitor for cancer therapy. |
| AID288527 | Binding affinity to human recombinant HSP90 assessed as inhibition of biotinylated-geldanamycin binding | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
| Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity. |
| AID395892 | Binding affinity to Hsp90 in human SKBR3 cells | 2009 | Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
| Discovery and development of heat shock protein 90 inhibitors. |
| AID1212925 | Metabolic stability in human liver microsomes at 5 uM by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
| AID745566 | Cytotoxicity against human ECA109 cells after 48 hrs by MTT assay | 2013 | Journal of natural products, May-24, Volume: 76, Issue:5
| Cytotoxic bisbenzylisoquinoline alkaloids from Stephania epigaea. |
| AID499308 | Antiproliferative activity against human A431 cells after 72 hrs | 2010 | Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
| Natural and semisynthetic azaphilones as a new scaffold for Hsp90 inhibitors. |
| AID506966 | Inhibition of HSP90-mediated antiapoptotic activity in human H69AR cells assessed as induction of PARP cleavage at 10 uM after 48 hrs by Western blot analysis | 2007 | Nature chemical biology, Aug, Volume: 3, Issue:8
| Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. |
| AID1184979 | Induction of heat shock response in human HCT116 cells assessed as HSP70 protein expression at IC50 level by western blotting method relative to untreated control | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
| Chemically accessible hsp90 inhibitor that does not induce a heat shock response. |
| AID421308 | Antiproliferative activity against human SK-MEL-5 cells after 72 to 144 hrs by cyquant DNA dye method | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. |
| AID1755752 | Antitumour activity against human SW-620 cells xenografted in Balb/c mouse assessed as decrease in Ki67 expression in tumour at 5 mg/kg, ip measured after 21 days immunochemical staining method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-((1-Phenyl-1H-1,2,3-triazol-4-yl)methyl)-2-azabicyclo[3.2.1]octan-3-one derivatives: Simplification and modification of aconitine scaffold for the discovery of novel anticancer agents. |
| AID421307 | Antiproliferative activity against human SW620 cells after 72 to 144 hrs by cyquant DNA dye method | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. |
| AID395896 | Inhibition of Hsp90 | 2009 | Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
| Discovery and development of heat shock protein 90 inhibitors. |
| AID506972 | Inhibition of HSP90-mediated antiapoptotic activity in human H69AR cells assessed as Akt inactivation at 10 uM after 24 hrs by Western blot analysis | 2007 | Nature chemical biology, Aug, Volume: 3, Issue:8
| Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. |
| AID465294 | Cmax in plasma of mouse bearing human A2780 cells at 80 mg/kg, ip administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID465301 | Apparent volume of distribution in tumor of mouse bearing human A2780 cells at 80 mg/kg, ip administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID1337020 | Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
| Design, synthesis and biological evaluation of 7-(aryl)-2,3-dihydro-[1,4]dioxino[2,3-g]quinoline derivatives as potential Hsp90 inhibitors and anticancer agents. |
| AID715181 | Inhibition of binding of recombinant HSP90 to his-tagged Akt up to 5 uM by Western blotting analysis | 2012 | Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
| An Hsp90 modulator that exhibits a unique mechanistic profile. |
| AID266546 | Inhibition of BODIPY-AG binding to human HSP90 | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
| Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. |
| AID266552 | Upregulation of Hsp70 in SKBR3 cells | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
| Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. |
| AID1128876 | Inhibition of human HSP90alpha expressed in yeast assessed as growth inhibition of host after 72 hrs | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Differences in conformational dynamics between Plasmodium falciparum and human Hsp90 orthologues enable the structure-based discovery of pathogen-selective inhibitors. |
| AID443321 | Growth inhibition of human PL45 cells at 250 nM after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID465293 | Binding affinity to HSP90 under non-reducing conditions in absence of TECP | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID429698 | Hepatotoxicity in ICR-SCID mouse liver assessed as bilirubin level at 100 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID443339 | Growth inhibition of human WS1 cells at 500 nM after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID1759980 | Inhibition of HSP90 (unknown origin) assessed as competition of fluorescently labelled geldanamycin binding after 2 hrs by microplate reader analysis | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Ring-opening of five-membered heterocycles conjugated 4-isopropylresorcinol scaffold-based benzamides as HSP90 inhibitors suppressing tumor growth in vitro and in vivo. |
| AID612788 | Inhibition of human Hsp90 interaction with FKBP52 protein using coomassie staining by Western blotting | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
| Synthesis and evaluation of biotinylated sansalvamide A analogs and their modulation of Hsp90. |
| AID465298 | AUC in tumor of mouse bearing human A2780 cells at 80 mg/kg, ip administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID1740809 | Binding affinity to HSP90 (unknown origin) | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Synthesis, structure and anticancer activity of new geldanamycin amine analogs containing C(17)- or C(20)- flexible and rigid arms as well as closed or open ansa-bridges. |
| AID710325 | Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition at 0.4 uM after 12 hrs by dual luciferase reporter gene assay in presence of dipyridol | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1α inhibitors. |
| AID394592 | Cytotoxicity against human MCF7 cells after 72 hrs in presence of NQO1 inhibitor dicoumarol | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
| AID465308 | Half life in liver of mouse bearing human A2780 cells at 80 mg/kg, ip administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID629769 | Antiproliferative activity against human CEM | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone. |
| AID745567 | Cytotoxicity against human A549 cells after 48 hrs by MTS assay | 2013 | Journal of natural products, May-24, Volume: 76, Issue:5
| Cytotoxic bisbenzylisoquinoline alkaloids from Stephania epigaea. |
| AID1187084 | Inhibition of HSP90 in human MDA-MB 231 cells assessed reduction in Raf protein levels at 0.5 uM by Western blot method | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors. |
| AID1212938 | Drug metabolism in human liver microsomes assessed as stability after 45 mins relative to control by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
| AID1334309 | Growth inhibition of human MCF7 cells at 10 uM after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
| Synthesis and in vitro antiproliferative activity of C5-benzyl substituted 2-amino-pyrrolo[2,3-d]pyrimidines as potent Hsp90 inhibitors. |
| AID664000 | Binding affinity to Hsp90 after 4 hrs by GM-FITC based fluorescence polarization assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Isoxazolo(aza)naphthoquinones: a new class of cytotoxic Hsp90 inhibitors. |
| AID1625290 | Inhibition of Hsp90 in human SKBR3 cells | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
| Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions. |
| AID629774 | Antitumor activity in mouse P388 cells xenografted in B6D2F1 mouse assessed as increase in mouse life span at 80 mg/kg/day, ip for 4 days relative to control | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone. |
| AID1310946 | Inhibition of HSP90 in human MCF7 cells assessed as ER-alpha protein degradation at 0.5 uM measured after 48 hrs by western blot analysis | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Novel 1,6-naphthyridin-2(1H)-ones as potential anticancer agents targeting Hsp90. |
| AID664003 | Cytotoxicity against human A431 cells after 72 hrs | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Isoxazolo(aza)naphthoquinones: a new class of cytotoxic Hsp90 inhibitors. |
| AID1187075 | Cytotoxicity against human LNCAP cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors. |
| AID1663550 | Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 30, Issue:15
| Enzymatic biosynthesis and biological evaluation of novel 17-AAG glucoside as potential anti-cancer agents. |
| AID1885314 | Inhibition of KDM4B (unknown origin) measured by AlphaScreen assay | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Recent Advances with KDM4 Inhibitors and Potential Applications. |
| AID288530 | Antiproliferative activity against human BT474 cells by MTS assay | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
| Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity. |
| AID1334306 | Growth inhibition of human HFF1 cells at 10 uM after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
| Synthesis and in vitro antiproliferative activity of C5-benzyl substituted 2-amino-pyrrolo[2,3-d]pyrimidines as potent Hsp90 inhibitors. |
| AID443328 | Growth inhibition of human HCT116 cells at 100 nM after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID732373 | Inhibition of Hsp90 in human MCF7 cells assessed as decrease in ErbB2 level at 0.1 uM after 24 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Synthesis and biological activities of a new class of heat shock protein 90 inhibitors, designed by energy-based pharmacophore virtual screening. |
| AID391038 | Toxicity in NMRI nu/nu mouse assessed as maximum tolerated dose | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Optimizing natural products by biosynthetic engineering: discovery of nonquinone Hsp90 inhibitors. |
| AID1187083 | Inhibition of HSP90 in human MDA-MB 231 cells assessed reduction in EGFR protein levels at 0.5 uM by Western blot method | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors. |
| AID1310936 | Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Novel 1,6-naphthyridin-2(1H)-ones as potential anticancer agents targeting Hsp90. |
| AID503293 | Inhibition of HSP90 expressed in HEK293 cells assessed as effect on Akt1:p27 interaction complexes by EYFP and/or YFP Venus fragment based reporter gene assay | 2006 | Nature chemical biology, Jun, Volume: 2, Issue:6
| Identifying off-target effects and hidden phenotypes of drugs in human cells. |
| AID1663546 | Solubility of the compound in water | 2020 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 30, Issue:15
| Enzymatic biosynthesis and biological evaluation of novel 17-AAG glucoside as potential anti-cancer agents. |
| AID1759979 | Antiproliferative activity against human HUVEC cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Ring-opening of five-membered heterocycles conjugated 4-isopropylresorcinol scaffold-based benzamides as HSP90 inhibitors suppressing tumor growth in vitro and in vivo. |
| AID629764 | Antiproliferative activity against human HCT15 | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone. |
| AID1184984 | Induction of heat shock response in human MIAPaCa2 cells assessed as HSF1 protein expression at IC50 level by western blotting method relative to untreated control | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
| Chemically accessible hsp90 inhibitor that does not induce a heat shock response. |
| AID421303 | Antiproliferative activity against human A375 cells after 72 to 144 hrs by cyquant DNA dye method | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. |
| AID201640 | In vitro inhibition of phospho-p185erbB-2 expression in human breast cancer cells(SK-BR-3 cells) at 200 mg/kg dose. | 1995 | Journal of medicinal chemistry, Sep-15, Volume: 38, Issue:19
| Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives. |
| AID314499 | Binding affinity at purified Hsp90 by DELFIA assay | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
| Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity. |
| AID465306 | Half life in plasma of mouse bearing human A2780 cells at 80 mg/kg, ip administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID242325 | Inhibitory concentration against ATPase activity of Hsp90 of Saccharomyces cerevisiae was determined by ATPase activity assay | 2005 | Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
| Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design. |
| AID288526 | Inhibition of human recombinant HSP90 in MCF7 cells assessed as Her2 degradation | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
| Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity. |
| AID288529 | Antiproliferative activity against human MCF7 cells by MTS assay | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
| Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity. |
| AID506974 | Inhibition of HSP90-mediated antiapoptotic activity in human WBA cells assessed as Akt inactivation at 10 uM after 24 hrs by Western blot analysis | 2007 | Nature chemical biology, Aug, Volume: 3, Issue:8
| Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. |
| AID1663549 | Antiproliferative activity against human SMMC7721 cells assessed as cell growth inhibition by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 30, Issue:15
| Enzymatic biosynthesis and biological evaluation of novel 17-AAG glucoside as potential anti-cancer agents. |
| AID443337 | Growth inhibition of human WS1 cells at 125 nM after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID506967 | Inhibition of HSP90-mediated antiapoptotic activity in human SKI-AC3 cells assessed as induction of PARP cleavage at 10 uM after 48 hrs by Western blot analysis | 2007 | Nature chemical biology, Aug, Volume: 3, Issue:8
| Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. |
| AID465310 | Ratio of drug level from tumor to plasma of mouse bearing human A2780 cells at 80 mg/kg, ip administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID629762 | Antiproliferative activity against human MX1 | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone. |
| AID421311 | Antiproliferative activity against human NCI-H460 cells after 72 to 144 hrs by cyquant DNA dye method | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. |
| AID745562 | Cytotoxicity against human SW480 cells after 48 hrs by MTS assay | 2013 | Journal of natural products, May-24, Volume: 76, Issue:5
| Cytotoxic bisbenzylisoquinoline alkaloids from Stephania epigaea. |
| AID53308 | Inhibition of DNA dependent protein kinase activity without hsp90 alpha protein | 2001 | Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
| LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family. |
| AID1212926 | Terminal half life in human | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
| AID465300 | Apparent volume of distribution in plasma of mouse bearing human A2780 cells at 80 mg/kg, ip administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID394602 | Cytotoxicity against human HCT116 cells after 72 hrs | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
| AID1167271 | Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors. |
| AID1128551 | Cell cycle arrest in human K562 cells assessed as accumulation at G1 phase at 1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors. |
| AID1663551 | Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 30, Issue:15
| Enzymatic biosynthesis and biological evaluation of novel 17-AAG glucoside as potential anti-cancer agents. |
| AID288536 | Selectivity index, ratio of IC50 for human RPTEC cells to IC50 for MCF7 cells | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
| Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity. |
| AID288535 | Selectivity index, ratio of IC50 for human RPTEC cells to IC50 for HT29 cells | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
| Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity. |
| AID288533 | Antiproliferative activity against human RPTEC | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
| Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity. |
| AID415527 | Induction of ERalpha degradation in human MCF7 cells at 1 uM after 24 hrs by Western blot analysis | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Integration of ligand and structure-based virtual screening for the identification of the first dual targeting agent for heat shock protein 90 (Hsp90) and tubulin. |
| AID629761 | Binding affinity to human Hsp90beta assessed as association constant after overnight incubation by fluorescence polarization assay | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone. |
| AID443318 | Growth inhibition of human PL45 cells at 1 nM after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID768700 | Cytotoxicity against human 7221 cells assessed as inhibition of cell replication after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and biological evaluation of pyrazolo[4,3-d]pyrimidine analogues. |
| AID1070516 | Binding affinity to recombinant HSP90-alpha (unknown origin) by surface plasmon resonance analysis | 2014 | Journal of natural products, Mar-28, Volume: 77, Issue:3
| Bioactive limonoids from the leaves of Azaridachta indica (Neem). |
| AID311911 | Growth inhibition of human HCT116 cells after 24 hrs by SRB assay | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
| 4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer. |
| AID267820 | Displacement of GM-BODIPY from Hsp90 | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis of Hsp90 dimerization modulators. |
| AID1187076 | Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors. |
| AID264093 | Inhibition of HSP90 ATPase activity | 2006 | Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
| 4-Amino derivatives of the Hsp90 inhibitor CCT018159. |
| AID1070515 | Inhibition of recombinant HSP90-alpha ATPase activity (unknown origin) at 2 to 50 uM after 60 mins by fluorimetric analysis | 2014 | Journal of natural products, Mar-28, Volume: 77, Issue:3
| Bioactive limonoids from the leaves of Azaridachta indica (Neem). |
| AID1175677 | Inhibition of Hsp90 chaperoning activity in rabbit reticulocyte lysate assessed as progesterone receptor hormone binding activity by liquid scintillation counting analysis | 2015 | Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1
| Bioactive metabolites from Chaetomium aureum: structure elucidation and inhibition of the Hsp90 machine chaperoning activity. |
| AID429694 | Hepatotoxicity in ICR-SCID mouse liver assessed as alkaline phosphatase level at 100 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID395897 | Inhibition of Hsp90 in human MCF7 cells assessed as Her2 degradation | 2009 | Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
| Discovery and development of heat shock protein 90 inhibitors. |
| AID768701 | Cytotoxicity against human 7402 cells assessed as inhibition of cell replication after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and biological evaluation of pyrazolo[4,3-d]pyrimidine analogues. |
| AID465281 | Inhibition of HSP90-mediated client protein HER2 degradation in human MCF7 cells | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID465305 | Clearance in liver of mouse bearing human A2780 cells at 80 mg/kg, ip administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID1212935 | Drug metabolism in human liver microsomes assessed as 17-aminogeldanamycin formation at 37 degC in presence of reduced GSH by liquid chromatography-tandem mass spectrometry | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
| AID1184968 | Inhibition of HSP90 in rabbit reticulocyte lysates at 100 nM pre-incubated for 5 hrs by firefly luciferase protein re-folding assay | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
| Chemically accessible hsp90 inhibitor that does not induce a heat shock response. |
| AID1663545 | Substrate activity at UDP-glycosyltransferase (unknown origin) assessed as enzyme-mediated metabolite formation in presence of UP-glucose by HPLC-LC/MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 30, Issue:15
| Enzymatic biosynthesis and biological evaluation of novel 17-AAG glucoside as potential anti-cancer agents. |
| AID465334 | Inhibition of HSP90alpha | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID1663552 | Antiproliferative activity against human SW480 cells assessed as cell growth inhibition by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 30, Issue:15
| Enzymatic biosynthesis and biological evaluation of novel 17-AAG glucoside as potential anti-cancer agents. |
| AID247222 | Inhibitory concentration against cell proliferation of human HCT116 cell | 2005 | Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
| Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design. |
| AID730648 | Binding affinity to recombinant Hsp90 alpha (unknown origin) by surface plasmon resonance | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
| A chemical-biological study reveals C9-type iridoids as novel heat shock protein 90 (Hsp90) inhibitors. |
| AID443335 | Growth inhibition of human WS1 cells at 1 nM after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID1167287 | Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors. |
| AID1185000 | Induction of apoptosis in human HCT116 cells at 1000 nM after 24 hrs by annexin V and 7-AAD staining based flow cytometry | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
| Chemically accessible hsp90 inhibitor that does not induce a heat shock response. |
| AID429688 | Hepatotoxicity in ICR-SCID mouse liver assessed as alanine aminotransferase level at 50 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID114902 | In vivo inhibition of phospho-p185erbB-2 expression in human SK-BR-3 tumors at 50 mg/kg dose in mice | 1995 | Journal of medicinal chemistry, Sep-15, Volume: 38, Issue:19
| Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives. |
| AID1128554 | Cell cycle arrest in human K562 cells assessed as reduction of S phase fraction at 1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors. |
| AID32535 | Inhibition of ATP-ase activity in human colon tumor cell line (HCT116) | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
| Adenine derived inhibitors of the molecular chaperone HSP90-SAR explained through multiple X-ray structures. |
| AID314504 | Growth inhibition of human DLD1 cells | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
| Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity. |
| AID465314 | Half life in human at 220 mg/m2 administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID629763 | Antiproliferative activity against human HCT116 | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone. |
| AID275011 | Apoptotic activity against JR8 cells after 72 hrs | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
| Small-molecule targeting of heat shock protein 90 chaperone function: rational identification of a new anticancer lead. |
| AID1708938 | Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
| Discovering High Potent Hsp90 Inhibitors as Antinasopharyngeal Carcinoma Agents through Fragment Assembling Approach. |
| AID324407 | Induction of light chain 3-GFP level in human H4 cells at 4.3 uM after 24 hrs by high throughput fluorescence microscopy relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
| Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
| AID1625307 | Inhibition of imatinib-resistant BCR-ABL T315I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as decrease in cell viability after 48 hrs by trypan blue exclusion assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
| Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions. |
| AID1740805 | Selectivity index, ratio of IC50 for cytotoxicity against human HDF cells to IC50 for cytotoxicity against human U-87 MG cells | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Synthesis, structure and anticancer activity of new geldanamycin amine analogs containing C(17)- or C(20)- flexible and rigid arms as well as closed or open ansa-bridges. |
| AID506965 | Inhibition of HSP90-mediated antiapoptotic activity in human WBA cells assessed as induction of caspase-3 cleavage at 10 uM after 48 hrs by Western blot analysis | 2007 | Nature chemical biology, Aug, Volume: 3, Issue:8
| Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. |
| AID1167282 | Cytotoxicity against human A549 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors. |
| AID1452317 | Antiproliferative activity against human H1299 cells after 48 hrs by resazurin dye-based fluorescence assay | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design and synthesis of neolamellarin a derivatives targeting heat shock protein 90. |
| AID465309 | Ratio of drug level from liver to plasma of mouse bearing human A2780 cells at 80 mg/kg, ip administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID604443 | Binding affinity to Hsp90alpha N-terminal ATPase domain by TR-FRET assay based competitive binding assay | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors. |
| AID620122 | Binding affinity to HSP90 | 2011 | Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
| Lead identification of β-lactam and related imine inhibitors of the molecular chaperone heat shock protein 90. |
| AID1708916 | Inhibition of HSP90-alpha (unknown origin) expressed in Escherichia coli BL21 assessed as reduction in ATPase activity at 10 uM in presence of PEP, NADH and ATP by pyruvate kinase/lactic dehydrogenase based coupled enzyme assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
| Discovering High Potent Hsp90 Inhibitors as Antinasopharyngeal Carcinoma Agents through Fragment Assembling Approach. |
| AID465283 | Inhibition of HSP90-mediated client protein HER2 degradation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID506584 | Binding affinity to HSP90 in human NCI-H526 cells at 1 uM after 24 hrs by fluorescence polarization assay | 2007 | Nature chemical biology, Aug, Volume: 3, Issue:8
| Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. |
| AID429686 | Hepatotoxicity in ICR-SCID mouse liver assessed as alanine aminotransferase level at 100 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID288534 | Antiproliferative activity against human HT29 cells | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
| Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity. |
| AID465364 | Antitumor activity against human NCI-H1650 cells xenografted in mouse at 100 mg/kg administered daily for 5 days a week | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID1708936 | Inhibition of HSP90-alpha (unknown origin) expressed in Escherichia coli BL21 assessed as reduction in ATPase activity in presence of PEP, NADH and ATP by pyruvate kinase/lactic dehydrogenase based coupled enzyme assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
| Discovering High Potent Hsp90 Inhibitors as Antinasopharyngeal Carcinoma Agents through Fragment Assembling Approach. |
| AID1752518 | Toxicity in BALB/c mouse xenografted with mouse 4T1 cells assessed as effect on body weight at 15 mg/kg, ip administered every 2 days starting from day 7 post-inoculation and measured on day 24 | 2021 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 50 | Total synthesis and biological evaluation of 7-hydroxyneolamellarin A as hypoxia-inducible factor-1α inhibitor for cancer therapy. |
| AID1334308 | Growth inhibition of human SKBR3 cells at 10 uM after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
| Synthesis and in vitro antiproliferative activity of C5-benzyl substituted 2-amino-pyrrolo[2,3-d]pyrimidines as potent Hsp90 inhibitors. |
| AID1663564 | Toxicity in nude mouse xenografted with human CNE2Z cells assessed as effect on body weight at 5 mg/kg, ip administered for 19 days | 2020 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 30, Issue:15
| Enzymatic biosynthesis and biological evaluation of novel 17-AAG glucoside as potential anti-cancer agents. |
| AID429796 | Growth inhibition of human tarceva and iressa-resistant HCC827 cells assessed as ATP level after 4 days | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID443325 | Growth inhibition of human HCT116 cells at 10 nM after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID257069 | Inhibition of cell proliferation in HCT116 human colon cancer cell line | 2005 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
| Structure-based discovery of a new class of Hsp90 inhibitors. |
| AID621858 | Binding affinity to human HSP90alpha assessed as 2D1H-15N chemical shift perturbation by NMR spectroscopy | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
| Lead generation of heat shock protein 90 inhibitors by a combination of fragment-based approach, virtual screening, and structure-based drug design. |
| AID201635 | In vitro inhibition of p185 erbB-2 oncoprotein in human breast cancer SK-BR-3 cells | 1995 | Journal of medicinal chemistry, Sep-15, Volume: 38, Issue:19
| erbB-2 oncogene inhibition by geldanamycin derivatives: synthesis, mechanism of action, and structure-activity relationships. |
| AID732358 | Inhibition of biotinylated geldanamycin binding to human recombinant Hsp90 ATP binding domain after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Synthesis and biological activities of a new class of heat shock protein 90 inhibitors, designed by energy-based pharmacophore virtual screening. |
| AID629766 | Antiproliferative activity against human NCI-H460 | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone. |
| AID240503 | Inhibition of yeast Hsp90 ATPase activity | 2005 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 15, Issue:14
| The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors. |
| AID1167285 | Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors. |
| AID392953 | Binding affinity to human full length Histidine6-tagged Hsp90alpha expressed in Escherichia coli BL21 DE3 by ITC | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
| 5-Aryl-4-(5-substituted-2,4-dihydroxyphenyl)-1,2,3-thiadiazoles as inhibitors of Hsp90 chaperone. |
| AID629756 | Binding affinity to human Hsp90beta after overnight incubation by fluorescence polarization assay | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone. |
| AID1310956 | Inhibition of HSP90 in human MCF7 cells assessed as induction of prosurvival heat shock response at 0.5 uM measured after 48 hrs by Western blot analysis | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Novel 1,6-naphthyridin-2(1H)-ones as potential anticancer agents targeting Hsp90. |
| AID443336 | Growth inhibition of human WS1 cells at 62.5 nM after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID429701 | Hepatotoxicity in ICR-SCID mouse liver assessed as bilirubin level at 75 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID377837 | Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-Glo assay | 2005 | Journal of natural products, Apr, Volume: 68, Issue:4
| Production of 8-demethylgeldanamycin and 4,5-epoxy-8-demethylgeldanamycin from a recombinant strain of Streptomyces hygroscopicus. |
| AID421314 | Inhibition of Hsp90 in human A375 cells assessed as Hsp70 induction after 24 hrs by high content screening | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. |
| AID620119 | Displacement of FITC-labeled geldanamycin from human recombinant HSP90alpha after 24 hrs by fluorescence displacement assay | 2011 | Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
| Lead identification of β-lactam and related imine inhibitors of the molecular chaperone heat shock protein 90. |
| AID421309 | Antiproliferative activity against human PC3 cells after 72 to 144 hrs by cyquant DNA dye method | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. |
| AID241892 | Inhibitory concentration against activity of Hsp90 was determined by fluorescence polarization (FP) assay | 2005 | Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
| Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design. |
| AID465302 | Apparent volume of distribution in liver of mouse bearing human A2780 cells at 80 mg/kg, ip administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID264092 | Inhibition of HSP90 by FP assay | 2006 | Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
| 4-Amino derivatives of the Hsp90 inhibitor CCT018159. |
| AID465304 | Clearance in tumor of mouse bearing human A2780 cells at 80 mg/kg, ip administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID266551 | Degradation of Her2 in SKOV3 cells | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
| Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. |
| AID1337018 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
| Design, synthesis and biological evaluation of 7-(aryl)-2,3-dihydro-[1,4]dioxino[2,3-g]quinoline derivatives as potential Hsp90 inhibitors and anticancer agents. |
| AID350568 | Binding affinity to human recombinant HSP90 | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Potent cytotoxic C-11 modified geldanamycin analogues. |
| AID1074618 | Inhibition of HSP90 in human CL1-5 cells assessed as reduction of slug expression after 16 hrs by Western blotting analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
| The antitumor agent PBT-1 directly targets HSP90 and hnRNP A2/B1 and inhibits lung adenocarcinoma growth and metastasis. |
| AID1885317 | Inhibition of KDM6B (unknown origin) measured by AlphaScreen assay | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Recent Advances with KDM4 Inhibitors and Potential Applications. |
| AID1128875 | Inhibition of human HSP90beta expressed in yeast assessed as growth inhibition of host after 72 hrs | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Differences in conformational dynamics between Plasmodium falciparum and human Hsp90 orthologues enable the structure-based discovery of pathogen-selective inhibitors. |
| AID275003 | Cytotoxicity against HeLa cells after 72 hrs | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
| Small-molecule targeting of heat shock protein 90 chaperone function: rational identification of a new anticancer lead. |
| AID275009 | Apoptotic activity against DU145 cells after 72 hrs | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
| Small-molecule targeting of heat shock protein 90 chaperone function: rational identification of a new anticancer lead. |
| AID350567 | Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-glo assay | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Potent cytotoxic C-11 modified geldanamycin analogues. |
| AID1755711 | Inhibition of recombinant human N terminal his-tagged HSP90 alpha (1 to 732 residues) expressed in Escherichia coli measured after 60 mins by Flourescence polarization assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-((1-Phenyl-1H-1,2,3-triazol-4-yl)methyl)-2-azabicyclo[3.2.1]octan-3-one derivatives: Simplification and modification of aconitine scaffold for the discovery of novel anticancer agents. |
| AID629772 | Antitumor activity in mouse P388 cells xenografted in B6D2F1 mouse assessed as median day of death at 80 mg/kg/day, ip for 4 days (Rvb = 10 days) | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone. |
| AID465307 | Half life in tumor of mouse bearing human A2780 cells at 80 mg/kg, ip administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID270492 | Displacement of cy3B-GM from Hsp90alpha | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
| Synthesis of a red-shifted fluorescence polarization probe for Hsp90. |
| AID465297 | AUC in plasma of mouse bearing human A2780 cells at 80 mg/kg, ip administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID443322 | Growth inhibition of human PL45 cells at 500 nM after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID612787 | Inhibition of human Hsp90 interaction with HOP protein using coomassie staining by Western blotting | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
| Synthesis and evaluation of biotinylated sansalvamide A analogs and their modulation of Hsp90. |
| AID1752516 | Antitumor activity against mouse 4T1 cells xenografted in BALB/c mouse assessed as tumor growth inhibition at 15 mg/kg, ip administered every 2 days starting from day 7 post-inoculation and measured on day 24 | 2021 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 50 | Total synthesis and biological evaluation of 7-hydroxyneolamellarin A as hypoxia-inducible factor-1α inhibitor for cancer therapy. |
| AID604446 | Inhibition of Hsp90alpha in human H1299 cells assessed as HIF-1alpha degradation by luciferase reporter assay | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors. |
| AID87634 | Binding affinity towards Heat shock protein HSP 90-alpha inhibitor | 2003 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22
| Synthesis of novel fluorescent probes for the molecular chaperone Hsp90. |
| AID710323 | Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition at 0.4 uM after 12 hrs by dual luciferase reporter gene assay in absence of dipyridol | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1α inhibitors. |
| AID443323 | Growth inhibition of human PL45 cells at 1000 nM after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID443329 | Growth inhibition of human HCT116 cells at 200 nM after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID394600 | Cytotoxicity against human SKBR3 cells after 72 hrs | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
| AID429797 | Growth inhibition of human tarceva and iressa-resistant NCI-H1975 cells assessed as ATP level after 4 days | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID1187080 | Inhibition of HSP90 in human MDA-MB 231 cells assessed reduction in CDK4 protein levels at 0.5 uM by Western blot method | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors. |
| AID429799 | Binding affinity to human HSP90alpha | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID288528 | Binding affinity to human recombinant HSP90 in MCF7 cell lysates assessed as inhibition of biotinylated-geldanamycin binding | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
| Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity. |
| AID1755712 | Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-((1-Phenyl-1H-1,2,3-triazol-4-yl)methyl)-2-azabicyclo[3.2.1]octan-3-one derivatives: Simplification and modification of aconitine scaffold for the discovery of novel anticancer agents. |
| AID767751 | Displacement of 5-(3-(3-(6-amino-8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9H-purin-9-yl)propyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from recombinant human Trap-1 after 24 hrs by fluorescence polarization assay | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series. |
| AID620120 | Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
| Lead identification of β-lactam and related imine inhibitors of the molecular chaperone heat shock protein 90. |
| AID1212927 | Total clearance in human | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4
| In vitro metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin in human liver microsomes. |
| AID465317 | Volume of distribution at steady state in human at 220 mg/m2 administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID506968 | Inhibition of HSP90-mediated antiapoptotic activity in human WBA cells assessed as induction of PARP cleavage at 10 uM after 48 hrs by Western blot analysis | 2007 | Nature chemical biology, Aug, Volume: 3, Issue:8
| Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. |
| AID443320 | Growth inhibition of human PL45 cells at 125 nM after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID266547 | Inhibition of BODIPY-AG binding to dog Grp94 | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
| Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. |
| AID394603 | Cytotoxicity against human MCF7 cells after 72 hrs | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
| AID395893 | Solubility in water | 2009 | Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
| Discovery and development of heat shock protein 90 inhibitors. |
| AID1184981 | Induction of heat shock response in human HCT116 cells assessed as HSF1 protein expression at IC50 level by western blotting method relative to untreated control | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
| Chemically accessible hsp90 inhibitor that does not induce a heat shock response. |
| AID429692 | Hepatotoxicity in ICR-SCID mouse liver assessed as aspartate aminotransferase level at 50 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID429779 | Toxicity in ICR-SCID mouse kidney assessed as creatinine level at 75 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID1167293 | Antitumor activity against human MDA-MB-231 cells xenografted in athymic nude mouse assessed as reduction in tumor weight at 10 mg/kg, iv dosed every 3 day for 15 consecutive days | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors. |
| AID429792 | Growth inhibition of human NCI-N87 cells assessed as ATP level after 4 days | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID629767 | Antiproliferative activity against human HT-29 | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone. |
| AID421305 | Antiproliferative activity against human MCF7 cells after 72 to 144 hrs by cyquant DNA dye method | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. |
| AID1167272 | Hepatotoxicity in Kunming mouse assessed as serum aspartate aminotransferase level at 10 mg/kg, iv (Rvb = 197.2 +/- 11.2 U/L) | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors. |
| AID465311 | Antitumor activity against human A2780 cells xenografted in mouse at 80 mg/kg, ip administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID1187082 | Inhibition of HSP90 in human MDA-MB 231 cells assessed reduction in Her2 protein levels at 0.5 uM by Western blot method | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors. |
| AID1310945 | Inhibition of HSP90 in human MCF7 cells assessed as Raf-1 protein degradation at 0.5 uM measured after 48 hrs by western blot analysis | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Novel 1,6-naphthyridin-2(1H)-ones as potential anticancer agents targeting Hsp90. |
| AID745564 | Cytotoxicity against human MCF7 cells after 48 hrs by MTS assay | 2013 | Journal of natural products, May-24, Volume: 76, Issue:5
| Cytotoxic bisbenzylisoquinoline alkaloids from Stephania epigaea. |
| AID1337019 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
| Design, synthesis and biological evaluation of 7-(aryl)-2,3-dihydro-[1,4]dioxino[2,3-g]quinoline derivatives as potential Hsp90 inhibitors and anticancer agents. |
| AID1708937 | Inhibition of HSP90-beta (unknown origin) expressed in Escherichia coli BL21 assessed as reduction in ATPase activity in presence of PEP, NADH and ATP by pyruvate kinase/lactic dehydrogenase based coupled enzyme assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
| Discovering High Potent Hsp90 Inhibitors as Antinasopharyngeal Carcinoma Agents through Fragment Assembling Approach. |
| AID1578154 | Antiproliferative activity against human HCT116 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression. |
| AID443338 | Growth inhibition of human WS1 cells at 250 nM after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID1184987 | Induction of heat shock response in human MIAPaCa2 cells assessed as HSP40 protein expression at IC50 level by western blotting method relative to untreated control | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
| Chemically accessible hsp90 inhibitor that does not induce a heat shock response. |
| AID1185003 | Induction of apoptosis in human HCT116 cells assessed as caspase 3/7 activation at 1000 nM after 24 hrs by luminometry | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
| Chemically accessible hsp90 inhibitor that does not induce a heat shock response. |
| AID421310 | Antiproliferative activity against human MDA-MB-231 cells after 72 to 144 hrs by cyquant DNA dye method | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. |
| AID1187081 | Inhibition of HSP90 in human MDA-MB 231 cells assessed increase in HSP70 protein levels at 0.5 and 5 uM by Western blot method | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors. |
| AID629765 | Antiproliferative activity against human PC3 | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone. |
| AID429689 | Hepatotoxicity in ICR-SCID mouse liver assessed as alanine aminotransferase level at 75 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID1625316 | Toxicity in human H1650 cells expressing E746-A750 EGFR deletion mutant xenografted in mouse administered ip 3 times per week | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
| Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions. |
| AID429705 | Toxicity in ICR-SCID mouse kidney assessed as BUN level at 75 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID275004 | Cytotoxicity against JR8 cells after 72 hrs | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
| Small-molecule targeting of heat shock protein 90 chaperone function: rational identification of a new anticancer lead. |
| AID1755713 | Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-((1-Phenyl-1H-1,2,3-triazol-4-yl)methyl)-2-azabicyclo[3.2.1]octan-3-one derivatives: Simplification and modification of aconitine scaffold for the discovery of novel anticancer agents. |
| AID1625306 | Inhibition of BCR-ABL (unknown origin) expressed in mouse BA/F3 cells assessed as decrease in cell viability after 48 hrs by trypan blue exclusion assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
| Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions. |
| AID715180 | Inhibition of binding of recombinant HSP90 to his-tagged HER2 up to 5 uM by Western blotting analysis | 2012 | Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
| An Hsp90 modulator that exhibits a unique mechanistic profile. |
| AID465319 | Toxicity in human assessed as maximum tolerated dose administered on 3 days schedule administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID314502 | Induction of human K562 cells differentiation | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
| Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity. |
| AID1755715 | Antiproliferative activity against human LoVo cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-((1-Phenyl-1H-1,2,3-triazol-4-yl)methyl)-2-azabicyclo[3.2.1]octan-3-one derivatives: Simplification and modification of aconitine scaffold for the discovery of novel anticancer agents. |
| AID1128547 | Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by trypan blue exclusion assay | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors. |
| AID767754 | Displacement of 5-(3-(3-(6-amino-8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9H-purin-9-yl)propyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from HSP90alpha (unknown origin) after 24 hrs by fluorescence polarization assay | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series. |
| AID715186 | Binding affinity to HSP90 in human HCT116 cells assessed as increase in staining intensity in cytosol at 200 uM after 24 hrs by immunofluorescence staining analysis | 2012 | Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
| An Hsp90 modulator that exhibits a unique mechanistic profile. |
| AID314501 | Inhibition of Hsp90 in human KPL4 cells assessed as depletion of Raf-1 level after 40 hrs | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
| Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity. |
| AID465282 | Chemical stability assessed as half life | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID506964 | Inhibition of HSP90-mediated antiapoptotic activity in human SKI-AC3 cells assessed as induction of caspase-3 cleavage at 10 uM after 48 hrs by Western blot analysis | 2007 | Nature chemical biology, Aug, Volume: 3, Issue:8
| Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. |
| AID275010 | Apoptotic activity against HeLa cells after 72 hrs | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
| Small-molecule targeting of heat shock protein 90 chaperone function: rational identification of a new anticancer lead. |
| AID429690 | Hepatotoxicity in ICR-SCID mouse liver assessed as aspartate aminotransferase level at 100 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID443340 | Growth inhibition of human WS1 cells at 1000 nM after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID201632 | Inhibition of oncogene product p185 erbB-2 from human breast cancer cells(SK-BR-3 cells) at 50 mg/kg dose. | 1995 | Journal of medicinal chemistry, Sep-15, Volume: 38, Issue:19
| Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives. |
| AID1720459 | Inhibition of HSP90 in human MCF7 cells assessed as Her2 protein expression level at IC50 after 24 hrs by ELISA (Rvb = 541.10 +/- 22.2 ng/ml) | 2020 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 30, Issue:15
| Quinazoline Based HSP90 Inhibitors: Synthesis, Modeling Study and ADME Calculations Towards Breast Cancer Targeting. |
| AID1752527 | Toxicity in BALB/c mouse xenografted with mouse 4T1 cells assessed as effect on liver morphology at 15 mg/kg, ip administered every 2 days starting from day 7 post-inoculation and measured on day 24 by Hematoxyin-eosin staining based analysis | 2021 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 50 | Total synthesis and biological evaluation of 7-hydroxyneolamellarin A as hypoxia-inducible factor-1α inhibitor for cancer therapy. |
| AID429697 | Hepatotoxicity in ICR-SCID mouse liver assessed as alkaline phosphatase level at 75 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID429700 | Hepatotoxicity in ICR-SCID mouse liver assessed as bilirubin level at 50 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID1184980 | Induction of heat shock response in human HCT116 cells assessed as HSP90 protein expression at IC50 level by western blotting method relative to untreated control | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
| Chemically accessible hsp90 inhibitor that does not induce a heat shock response. |
| AID506973 | Inhibition of HSP90-mediated antiapoptotic activity in human SKI-AC3 cells assessed as Akt inactivation at 10 uM after 24 hrs by Western blot analysis | 2007 | Nature chemical biology, Aug, Volume: 3, Issue:8
| Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. |
| AID275002 | Cytotoxicity against DU145 cells after 72 hrs | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
| Small-molecule targeting of heat shock protein 90 chaperone function: rational identification of a new anticancer lead. |
| AID1318681 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Design and synthesis of N-(5-chloro-2,4-dihydroxybenzoyl)-(R)-1,2,3,4-tetrahydroisoquinoline-3-carboxamides as novel Hsp90 inhibitors. |
| AID394611 | Antitumor activity against human COLO205 tumor bearing mouse assessed as reduction of tumor volume at 15 mg/kg, iv once daily for 5 days with 2 day interval for total 13 doses | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
| AID465296 | Cmax in liver of mouse bearing human A2780 cells at 80 mg/kg, ip administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID1726507 | Binding affinity to recombinant N-terminal His6-tagged HSP90 NM-domain (unknown origin) (1 to 226 residues) expressed in Escherichia coli BL21 (DE3) (DNAY) cells assessed as chemical shift perturbation at protein to compound ratio of 1:1 by 15N-1H TROSY-H | 2021 | RSC medicinal chemistry, Mar-01, Volume: 12, Issue:3
| Using NMR to identify binding regions for N and C-terminal Hsp90 inhibitors using Hsp90 domains. |
| AID465303 | Clearance in plasma of mouse bearing human A2780 cells at 80 mg/kg, ip administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID1752528 | Toxicity in BALB/c mouse xenografted with mouse 4T1 cells assessed as effect on spleen morphology at 15 mg/kg, ip administered every 2 days starting from day 7 post-inoculation and measured on day 24 by Hematoxyin-eosin staining based analysis | 2021 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 50 | Total synthesis and biological evaluation of 7-hydroxyneolamellarin A as hypoxia-inducible factor-1α inhibitor for cancer therapy. |
| AID429708 | Toxicity in ICR-SCID mouse kidney assessed as creatinine level at 50 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID1167275 | Inhibition Hsp90 in human MDA-MB 231 cells assessed as increase in HSP70 protein level at 0.5 uM incubated for 24 hrs by Western blot method | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors. |
| AID421306 | Antiproliferative activity against human HT-29 cells after 72 to 144 hrs by cyquant DNA dye method | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. |
| AID1708915 | Binding affinity to HSP90-alpha (unknown origin) expressed in Escherichia coli BL21 by SPR assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
| Discovering High Potent Hsp90 Inhibitors as Antinasopharyngeal Carcinoma Agents through Fragment Assembling Approach. |
| AID629768 | Antiproliferative activity against mouse B16F10 | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone. |
| AID429787 | Toxicity in ICR-SCID mouse heart assessed as cholesterol level at 75 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID1759977 | Antiproliferative activity against human Hep3B cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Ring-opening of five-membered heterocycles conjugated 4-isopropylresorcinol scaffold-based benzamides as HSP90 inhibitors suppressing tumor growth in vitro and in vivo. |
| AID629758 | Antiproliferative activity against human SKBR3 | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone. |
| AID1740796 | Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Synthesis, structure and anticancer activity of new geldanamycin amine analogs containing C(17)- or C(20)- flexible and rigid arms as well as closed or open ansa-bridges. |
| AID264094 | Antiproliferative activity against HCT116 cell line | 2006 | Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
| 4-Amino derivatives of the Hsp90 inhibitor CCT018159. |
| AID1708935 | Binding affinity to HSP90-beta (unknown origin) expressed in Escherichia coli BL21 by SPR assay | 2021 | Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
| Discovering High Potent Hsp90 Inhibitors as Antinasopharyngeal Carcinoma Agents through Fragment Assembling Approach. |
| AID324563 | Increase in light chain 3-GFP+ autophagosome vesicle intensity per cell in human H4 cells at 4.3 uM after 24 hrs by high throughput fluorescence microscopy relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
| Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
| AID1167283 | Cytotoxicity against human HeLa cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors. |
| AID1885316 | Inhibition of KDM5A (unknown origin) measured by AlphaScreen assay | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
| Recent Advances with KDM4 Inhibitors and Potential Applications. |
| AID443317 | Growth inhibition of human PL45 cells after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID1128874 | Inhibition of Plasmodium falciparum HSP90 K313Q mutant expressed in yeast assessed as growth inhibition of host after 72 hrs | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Differences in conformational dynamics between Plasmodium falciparum and human Hsp90 orthologues enable the structure-based discovery of pathogen-selective inhibitors. |
| AID1759976 | Antiproliferative activity against human HCT116 cells assessed as growth inhibition incubated for 48 hrs by Sulforhodamine B assay | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Ring-opening of five-membered heterocycles conjugated 4-isopropylresorcinol scaffold-based benzamides as HSP90 inhibitors suppressing tumor growth in vitro and in vivo. |
| AID1740806 | Selectivity index, ratio of IC50 for cytotoxicity against human HDF cells to IC50 for cytotoxicity against human A549 cells | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Synthesis, structure and anticancer activity of new geldanamycin amine analogs containing C(17)- or C(20)- flexible and rigid arms as well as closed or open ansa-bridges. |
| AID1128548 | Induction of apoptosis in human K562 cells assessed as hypoploid nuclei accumulated in sub-G0-G1 phase after 30 mins by propidium iodide staining-based fluorescence microscopic analysis | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | 4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors. |
| AID307450 | Cell viability of mouse P19 derived neurons at 1 nM by XTT reduction assay relative to control | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Geldanamycin derivatives and neuroprotective effect on cultured P19-derived neurons. |
| AID1578156 | Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression. |
| AID1625308 | Inhibition of imatinib-resistant BCR-ABL E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as decrease in cell viability after 48 hrs by trypan blue exclusion assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
| Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions. |
| AID611482 | Inhibition of intrinsic ATPase activity of human Hsp90 alpha assessed as inorganic phosphate release after ATP hydrolysis at 100 uM by colorimetric malachite green assay | 2011 | Journal of natural products, Jun-24, Volume: 74, Issue:6
| Chaxamycins A-D, bioactive ansamycins from a hyper-arid desert Streptomyces sp. |
| AID1755716 | Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-((1-Phenyl-1H-1,2,3-triazol-4-yl)methyl)-2-azabicyclo[3.2.1]octan-3-one derivatives: Simplification and modification of aconitine scaffold for the discovery of novel anticancer agents. |
| AID421312 | Antiproliferative activity against human HCT15 cells after 72 to 144 hrs by cyquant DNA dye method | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. |
| AID1452315 | Inhibition of FITC-GA binding to HSP90alpha (unknown origin) at 0.5 uM by fluorescence polarization assay | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design and synthesis of neolamellarin a derivatives targeting heat shock protein 90. |
| AID1720460 | Inhibition of HSP90 in human MCF7 cells assessed as HSP70 protein expression level at IC50 after 24 hrs by ELISA (Rvb = 9.836 +/- 1.21 ng/ml) | 2020 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 30, Issue:15
| Quinazoline Based HSP90 Inhibitors: Synthesis, Modeling Study and ADME Calculations Towards Breast Cancer Targeting. |
| AID429786 | Toxicity in ICR-SCID mouse heart assessed as cholesterol level at 50 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID1625317 | Toxicity in human H1975 cells xenografted in mouse administered ip 3 times per week | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
| Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions. |
| AID1625291 | Ratio of IC50 for inhibition of Hsp90 in human RPTEC cells to IC50 for human BT474 cells | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
| Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions. |
| AID429783 | Toxicity in ICR-SCID mouse heart assessed as creatine phospholipase level at 75 mg/kg administered 3 times per week for 4 weeks measured after 24 hrs of last dose relative to untreated control | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID1755720 | Cytotoxicity against human NCM460 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-((1-Phenyl-1H-1,2,3-triazol-4-yl)methyl)-2-azabicyclo[3.2.1]octan-3-one derivatives: Simplification and modification of aconitine scaffold for the discovery of novel anticancer agents. |
| AID443326 | Growth inhibition of human HCT116 cells at 20 nM after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID266548 | Inhibition of human SKBR3 cell growth | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
| Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. |
| AID443327 | Growth inhibition of human HCT116 cells at 50 nM after 24 hrs by [3H]thymidine uptake assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action. |
| AID429789 | Growth inhibition of human BT474 cells assessed as ATP level after 4 days | 2009 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
| Synthesis of pochoxime prodrugs as potent HSP90 inhibitors. |
| AID1184983 | Induction of heat shock response in human HCT116 cells assessed as HSP27 protein expression at IC50 level by western blotting method relative to untreated control | 2014 | ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
| Chemically accessible hsp90 inhibitor that does not induce a heat shock response. |
| AID465292 | Solubility in water | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID324459 | Increase in light chain 3-GFP+ autophagosome vesicle number per cell in human H4 cells at 4.3 uM after 24 hrs by high throughput fluorescence microscopy relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
| Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
| AID506585 | Inhibition of HSP90-mediated proliferation of human NCI-H526 cells at 1 uM after 96 hrs by sulforhodamine B assay | 2007 | Nature chemical biology, Aug, Volume: 3, Issue:8
| Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. |
| AID1740798 | Antiproliferative activity against human PC-3 cells assessed as reduction in cell growth incubated for 72 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Synthesis, structure and anticancer activity of new geldanamycin amine analogs containing C(17)- or C(20)- flexible and rigid arms as well as closed or open ansa-bridges. |
| AID314506 | Growth inhibition of human KPL4 cells | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
| Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity. |
| AID421302 | Binding affinity to pig spleen Hsp90 ATPase pocket by Bradford assay | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. |
| AID465295 | Cmax in tumor of mouse bearing human A2780 cells at 80 mg/kg, ip administered as DMSO/egg phospholipid formulation | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Heat shock protein 90: inhibitors in clinical trials. |
| AID1192911 | Efflux ratio of permeability from basolateral to apical side over apical to basolateral side in MDCK-MDR1 cells | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Discovery of novel oxazepine and diazepine carboxamides as two new classes of heat shock protein 90 inhibitors. |
| AID732372 | Inhibition of Hsp90 in human MCF7 cells assessed as decrease in cRAF level at 0.1 uM after 24 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Synthesis and biological activities of a new class of heat shock protein 90 inhibitors, designed by energy-based pharmacophore virtual screening. |
| AID1755717 | Cytotoxicity against human MRC5 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | 2-((1-Phenyl-1H-1,2,3-triazol-4-yl)methyl)-2-azabicyclo[3.2.1]octan-3-one derivatives: Simplification and modification of aconitine scaffold for the discovery of novel anticancer agents. |
| AID604503 | Inhibition of Hsp90alpha in human SKBR3 cells assessed as up-regulation of HSP70 protein by Western blot analysis | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors. |
| AID1167281 | Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors. |
| AID506962 | Inhibition of HSP90-mediated antiapoptotic activity in human WBA cells assessed as increase in caspase-3 activity at 10 uM after 48 hrs by Western blot analysis | 2007 | Nature chemical biology, Aug, Volume: 3, Issue:8
| Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. |
| AID243471 | Inhibition of yeast Hsp90 ATPase activity at 40 uM | 2005 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 15, Issue:14
| The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors. |
| AID1188656 | Toxicity in patient assessed as median survival time at 450 mg/m'2, iv administered per week | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Progress in the discovery and development of heat shock protein 90 (Hsp90) inhibitors. |
| AID87633 | Competitive binding towards Heat shock protein HSP 90-alpha | 2001 | Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
| LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family. |
| AID394604 | Cytotoxicity against NQ01-deficient human MDA468 cells after 72 hrs | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus. |
| AID506970 | Inhibition of HSP90-mediated antiapoptotic activity in human SKI-AC3 cells assessed as increase in caspase-7 activity at 10 uM after 48 hrs by Western blot analysis | 2007 | Nature chemical biology, Aug, Volume: 3, Issue:8
| Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer. |
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
| Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| AID1347415 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: tertiary screen by RT-qPCR | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347414 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
| Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
| AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3
| High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
| AID1801076 | Fluorescence Polarization Assay (FPA) from Article 10.1111/cbdd.12371: \\Discovery of novel 17-phenylethylaminegeldanamycin derivatives as potent Hsp90 inhibitors.\\ | 2015 | Chemical biology & drug design, Feb, Volume: 85, Issue:2
| Discovery of novel 17-phenylethylaminegeldanamycin derivatives as potent Hsp90 inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |